新项目精选

近年来，药物发现已从传统的小分子化药拓展至更多元的分子类型，这些新型API在项目整合中呈现出独特的开发范式：PROTAC/分子胶降解剂：通过诱导靶蛋白泛素化降解发挥作用，而非传统“占位驱动”抑制。这类分子的项目整合需要同时考量靶点配体、E3连接酶配体及连接子的三元复合物优化，临床前到临床的转化难度显著增加。多肽/环肽药物：介于小分子与生物制品之间，兼具高选择性与口服可用性潜力。项目整合中需重点解决稳定性、递送及生产工艺放大问题。抗体-药物偶联物（ADC）：作为“生物导弹”，ADC的项目整合涉及抗体、连接子、有效载荷三部分的协同优化，需要跨学科团队的深度整合。小核酸药物（siRNA/ASO）：通过基因沉默机制发挥作用，项目整合的核心挑战在于递送系统的设计与肝外靶向能力的突破。展望未来，新型API项目的整合将呈现以下趋势：第一，AI贯穿全链条。从靶点发现、分子优化到临床开发、上市后监测，AI将成为贯穿API全生命周期的核心工具。第二，数据资产化。临床研究数据和真实世界数据将从“辅助工具”升级为“核心资产”，数据驱动的决策将成为项目整合的标准范式。第三，开放整合生态。API经济的成熟正在推动制药企业从“封闭研发”走向“开放协作”，通过API接口与外部数据源、技术平台、CRO/CDMO实现无缝对接. 而API技术——无论是数据接口还是组织协作的“应用程序接口”——正成为支撑这一整合的核心基础设施。
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新项目整合精选

新产品编号:1944787

Chemical Name: 1-(4-Chlorophenyl)-3-[2-(diethylaminoethyl)amino]-6-hydroxy-2(Z)-hexen-1-one
项目整合开发状态: Preclinical
项目研究机构: Central Drug Research Institute (Originator)
合成路线:Acetophenone (I) is...
参考文献标题:Syntheses and biological evaluation of 3-substituted amino-1-aryl-6-hydroxy-hex-2-ene-1-ones as antioxidant and hypolipidemic agents
文献作者:Batra,S.; Srivastava,S.K.; Singh,K.; Chander,R.; Khanna,A.K.; Bhaduri,A.P.
参考来源:Bioorg Med Chem 2000,8(8),2195

LY-339687

Chemical Name: 4-(1-Ethylpropylidene)-L-glutamic acid
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator), NPS Allelix (Originator)
合成路线:Treatment of ethyl N-Boc-(S)-pyroglutamate (I) wit...
参考文献标题:Glutamic acid derivs.and pharmaceutical compsns.for the treatment of central nervous system disorders
文献作者:Rubio Esteban,A.; Pedregal Tercero,C.(Lilly SA)
参考来源:EP 0867430; ES 2133095; JP 1998279542

PHD-321

Chemical Name: N-[1-Benzyl-2-[1-(1-naphthyl)ethylamino]ethyl]-3,4-dimethoxybenzenesulfonamide hydrochloride
项目整合开发状态: Biological Testing
项目研究机构: CNRS (Originator)
合成路线:The condensation of all...
参考文献标题:Aralkyl-1,2-diamines having calcimimetic activity and preparation mode
文献作者:Potier,P.J.-P.S.J.; Ruat,M.; Dauban,P.M.; Faure,H.V.; Dodd,R.(CNRS (Centre National de la Recherche Scientifique))
参考来源:WO 0134562

CP-5068

Chemical Name: (1S,5R,6S)-2-[6-(Carbamoylmethyl)-7-(methylsulfanyl)imidazo[5,1-b]thiazol-6-ium-2-yl]-6-[1(R)-hydroxyethyl]-1-methyl-1-carba-2-penem-3-carboxylate
项目整合开发状态: Preclinical
项目研究机构: Me...
参考文献标题:Process for synthesizing carbapenem intermediates using a rhodium catalyst and Lewis acid
文献作者:Lynch,J.E.; Liu,T.M.-H.; Volante,R.P.(Merck & Co.,Inc.)
参考来源:US 5493018

JNJ-2408068, R-170591

Chemical Name: 2-[2-[1-(2-Aminoethyl)piperidin-4-ylamino]-4-methyl-1H-benzimidazol-1-ylmethyl]-6-methylpyridin-3-ol
项目整合开发状态: Preclinical
项目研究机构: Janssen (Originator)
合成路线:Condensation of eth...
参考文献标题:Respiratory syncytial virus replication inhibitors
文献作者:Sommen,F.M.; Andries,K.J.L.M.; Guillemont,J.E.G.; Lacrampe,J.F.A.; Janssens,F.E.; Meersman,K.P.M.-J.(Janssen Pharmaceutica NV)
参考来源:WO 0100611

MC-04,546, RWJ-333441

Chemical Name: (6R,7R)-7-[2-(5-Amino-1,2,4-thiadiazol-3-yl)-2(Z)-(hydroxyimino)acetamido]-3-[2-(2-ammonioethyl)sulfanylmethyl]pyridin-3-ylsulfanyl]-3-cephem-4-carboxylate
项目整合开发状态: Preclinical
项...
参考文献标题:Discovery of novel anti-MRSA cephalosporin RWJ-333441 (MC-04,546).Relationships between structure,antibacterial activity,serum stability,pharmacokinetics and efficacy in a series of (3-heteroarylthio)cephems
文献作者:Griffith,D.; Blais,J.; Hevker,S.; Price,M.; Huie,K.; Halas,S.; Cho,A.; Dudley,M.; Lee,V.; Ludwikow,M.; Chen,S.; Chemberland,S.; Glinka,T.
参考来源:40th Intersci Conf Antimicrob Agents Chemother (Sept 17 2000,Toronto) 2000,Abst F-1071

MC-04,699, RWJ-333442

Chemical Name: (6R,7R)-7-[2-(5-Amino-1,2,4-thiadiazol-3-yl)-2(Z)-(hydroxyimino)acetamido]-3-[2-[2-(L-aspartylamino)ethyl]sulfanylmethyl]pyridin-3-ylsulfanyl]-3-cephem-4-carboxylic acid
项目整合开发状态: Pr...
参考文献标题:Discovery of novel anti-MRSA cephalosporin RWJ-333441 (MC-04,546).Relationships between structure,antibacterial activity,serum stability,pharmacokinetics and efficacy in a series of (3-heteroarylthio)cephems
文献作者:Griffith,D.; Blais,J.; Hevker,S.; Price,M.; Huie,K.; Halas,S.; Cho,A.; Dudley,M.; Lee,V.; Ludwikow,M.; Chen,S.; Chemberland,S.; Glinka,T.
参考来源:40th Intersci Conf Antimicrob Agents Chemother (Sept 17 2000,Toronto) 2000,Abst F-1071

AP-5280

Chemical Name: cis-Diammine platinum complex polymer composed of an HMPA copolymer bound to an amidomalonate chelator through a Gly-Phe-Leu-Gly linker
项目整合开发状态: Phase I/II
项目研究机构: Access Pharmac...
参考文献标题:Polymer-platinum cpds.
文献作者:Duncan,R.; Evagorou,E.G.; Buckley,R.G.; Gianasi,E.(Access Pharmaceuticals,Inc.)
参考来源:WO 9847537

RU-84687

Chemical Name: N2-Acetyl-N1-[1-(biphenyl-4-ylmethyl)-2-oxoperhydroazepin-3(S)-yl]-3-formyl-4-O-phosphono-L-tyrosinamide
项目整合开发状态: Biological Testing
项目研究机构: Aventis Pharma (Originator)
合成路线:A...
参考文献标题:SAR and rational design of Src SH2 binders around a heterocyclic scaffold identification of RU84687,a subnanomolar and Src SH2 selective binder
文献作者:Mandine,E.; Baholet,I.; Deprez,P.; et al.
参考来源:16th Int Symp Med Chem (Sept 18 2000,Bologna) 2000,Abst PA-17

DV-182

Chemical Name: 8-[2-[4-(2,5-Dichlorophenyl)piperazin-1-yl]-1-methylethyl]-8-azaspiro[4.5]decane-7,9-dione
项目整合开发状态: Biological Testing
项目研究机构: Recordati (Originator)
合成路线:Mitsunobu coupling o...
参考文献标题:Cyclic amides and imides having selective antagonist activity at alpha-1D adrenergic receptor
文献作者:Testa,R.; Leonardi,A.; Motta,G.; Barlocco,D.(Recordati Industria Chimica e Farmaceutica SpA)
参考来源:WO 0105765